In vitro activity of artemisinin, its derivatives, and pyronaridine against different strains of Plasmodium falciparum.
The activities of artemisinin (qinghaosu), dihydroartemisinin (dihydroqinghaosu), artemether and pyronaridine were tested in a 48 h in vitro assay against 3 chloroquine-sensitive and one chloroquine-resistant strains of Plasmodium falciparum. Growth inhibition was modelled with a sigmoid Emax model. All compounds markedly inhibited the growth of all strains although, for the chloroquine-resistant strain, merozoites were detected at concentrations as high as 10(-4) M of artemisinin, dihydroartemisinin and artemether. Dihydroartemisinin, artemether and pyronaridine appeared to be more potent than artemisinin, with EC50 values of 4.7-23 nM, 0.98-6.1 nM and 4.4-18 nM respectively, while the EC50 value of artemisinin was 3-108 nM against all 4 strains.
Alin
M H
MH
Department of Morphology and Pathology, Faculty of Medicine, Somali National University, Mugadishu.
Björkman
A
A
Ashton
M
M
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D000077549:Artemether; D037621:Artemisinins; D004305:Dose-Response Relationship, Drug; D004351:Drug Resistance; D066298:In Vitro Techniques; D009287:Naphthyridines / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development; D012717:Sesquiterpenes / Q000494:pharmacology*
D000962:Antimalarials; D037621:Artemisinins; D009287:Naphthyridines; D012717:Sesquiterpenes; C039060:artenimol; C031327:artemisinin; D000077549:Artemether; C027871:pyronaridine